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[PMID]:28403892
[Au] Autor:Qazi F; Shoaib MH; Yousuf RI; Nasiri MI; Ahmed K; Ahmad M
[Ad] Endereço:Department of Pharmaceutics, Faculty of Pharmacy & Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.
[Ti] Título:Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent-Meclizine HCl.
[So] Source:Lipids Health Dis;16(1):75, 2017 Apr 12.
[Is] ISSN:1476-511X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Antiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. METHODS: Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol ), Glyceryl palmitostearate (Precirol ), Glyceryl behenate (Compritol ) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5-1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. RESULTS: Sphericity indicated by shape factor (e ) varied with type and concentration of lipids: Geleol (e = 0.891-0.997), Precirol (e = 0.611-0.743), Compritol (e = 0.665-0.729) and Carnauba wax (e = 0.499-0.551). Highly spherical pellets were obtained with Geleol (Aspect ratio = 1.005-1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153-1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol and Compritol , (ii) Geleol and Carnauba wax and (iii) Geleol , Compritol and Carnauba wax. Scanning electron microscopy of Compritol pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol and Compritol pellets, explained by Korsmeyer-Peppas (R = 0.978-0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol and Carnauba wax and (iii) Geleol , Compritol and Carnauba wax pellets followed Zero-order (R = 0.991-0.995). Similarity test was performed using combination of Geleol and Compritol (i) as a reference. CONCLUSIONS: Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol , Compritol and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.
[Mh] Termos MeSH primário: Antieméticos/administração & dosagem
Ácidos Graxos/química
Glicerídeos/química
Lipídeos/química
Meclizina/administração & dosagem
Veículos Farmacêuticos/química
Ceras/química
[Mh] Termos MeSH secundário: Administração Oral
Antieméticos/química
Preparações de Ação Retardada/administração & dosagem
Preparações de Ação Retardada/química
Diglicerídeos/química
Composição de Medicamentos
Liberação Controlada de Fármacos
Estabilidade de Medicamentos
Armazenamento de Medicamentos
Seres Humanos
Concentração de Íons de Hidrogênio
Meclizina/química
Microscopia Eletrônica de Varredura
Solubilidade
Espectroscopia de Infravermelho com Transformada de Fourier
Água/análise
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiemetics); 0 (Delayed-Action Preparations); 0 (Diglycerides); 0 (Fatty Acids); 0 (Glycerides); 0 (Lipids); 0 (Pharmaceutical Vehicles); 0 (Waxes); 059QF0KO0R (Water); 18641-57-1 (glyceryl behenate); 230OU9XXE4 (glyceryl monostearate); 3L5TQ84570 (Meclizine); GSY51O183C (precirol); R12CBM0EIZ (carnauba wax)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170414
[St] Status:MEDLINE
[do] DOI:10.1186/s12944-017-0466-x


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[PMID]:28118132
[Au] Autor:Habib NM; Abdelrahman MM; Abdelwhab NS; Ali NW
[Ad] Endereço:Beni-Suef University, Faculty of Pharmacy, Pharmaceutical Analytical Chemistry Department, Alshaheed Shehata Ahmed Hegazy St, Beni-Suef 62514, Egypt.
[Ti] Título:Validated Chromatographic Methods for the Analysis of Two Binary Mixtures Containing Pyridoxine Hydrochloride.
[So] Source:J AOAC Int;100(2):414-421, 2017 Mar 01.
[Is] ISSN:1060-3271
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Accurate and precise TLC-densitometric and HPLC-diode-array detector (DAD) methods have been developed and validated to resolve two binary mixtures containing pyridoxine hydrochloride (PYH) with either cyclizine hydrochloride (CYH) or meclizine hydrochloride (MEH). In the developed TLC-densitometric method, chromatographic separation of the three studied drugs was carried out on silica gel 60 F254 plates using a developing system containing methylene chloride + acetone + methanol (7 + 1 + 0.5, v/v/v) scanning separated bands at 220 nm. Beer-Lambert law was obeyed in the ranges of 0.2-5, 0.2-4, and 0.2-4 µg/band for PYH, CYH, and MEH, respectively. On the other hand, the developed HPLC-DAD method depended on chromatographic separation on a Zorbax Eclipse C18 column using methanol-KH2PO4 (0.05 M; 90 + 10, v/v; pH 5, with H3PO4 and KOH) as the mobile phase, a flow rate of 1 mL/min, and UV scanning at 220 nm. A linear relationship was obtained between the integrated peak area and the concentration in the ranges of 10-50, 10-50, and 7-50 µg/mL for PYH, CYH, and MEH, respectively. The proposed methods were successfully applied for the determination of the cited drugs in their pharmaceutical formulations. Statistical comparison with the reported methods using Student's t- and F-tests found there were no significant differences between the proposed and reported methods for accuracy and precision.
[Mh] Termos MeSH primário: Cromatografia de Fase Reversa/métodos
Cromatografia em Camada Delgada/métodos
Densitometria/métodos
Piridoxina/análise
[Mh] Termos MeSH secundário: Ciclizina/análise
Acurácia dos Dados
Combinação de Medicamentos
Meclizina/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Drug Combinations); 0 (dizerest B6); 0 (emetrex); 3L5TQ84570 (Meclizine); KV2JZ1BI6Z (Pyridoxine); QRW9FCR9P2 (Cyclizine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170606
[Lr] Data última revisão:
170606
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170125
[St] Status:MEDLINE
[do] DOI:10.5740/jaoacint.16-0213


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[PMID]:28081025
[Au] Autor:Chowdhury NA; Sewatsky ML; Kim H
[Ad] Endereço:From the New York-Presbyterian Hospital/Weill Cornell Medical Center, Weill Cornell Medicine (NAC); and NewYork-Presbyterian Hospital/Columbia University Medical Center, Columbia University College of Physicians & Surgeons (MLS, HK), New York, New York.
[Ti] Título:Transdermal Scopolamine Withdrawal Syndrome Case Report in the Pediatric Cerebral Palsy Population.
[So] Source:Am J Phys Med Rehabil;96(8):e151-e154, 2017 Aug.
[Is] ISSN:1537-7385
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Sialorrhea in children with cerebral palsy (CP) results in aspiration, decreased social integration, and poor quality of life. Management options include transdermal anticholinergics such as the scopolamine patch. A controlled clinical trial has proven botulinum toxin (BTX) injections into the salivary glands are an effective alternative to transdermal anticholinergics with a safer side effect profile. Multiple studies of the injections in diverse populations demonstrate reduction in saliva production with improvement in quality of life and decrease in hospitalization-associated costs. The authors describe a 15-year-old boy with spastic quadriplegic CP who developed emesis, nausea, and lethargy 1 day after the first injection of botulinum toxin A (BTX-A) to his salivary glands for sialorrhea management. The authors ascribed his symptoms to scopolamine withdrawal. Given the lack of exposure in the medical literature, there is minimal awareness of the withdrawal syndrome from transdermal scopolamine in children with or without CP, resulting in delayed diagnosis and potential complications. Treatment of the withdrawal syndrome has been successful with meclizine though safety and efficacy has not been established in children younger than 12 despite frequent clinical and over-the-counter use. Prompt diagnosis of the transdermal scopolamine withdrawal syndrome can result in quicker treatment and a shorter hospital stay.
[Mh] Termos MeSH primário: Paralisia Cerebral/complicações
Diagnóstico Tardio/efeitos adversos
Hidrobrometo de Escopolamina/efeitos adversos
Sialorreia/tratamento farmacológico
Síndrome de Abstinência a Substâncias/diagnóstico
[Mh] Termos MeSH secundário: Adolescente
Antieméticos/uso terapêutico
Toxinas Botulínicas Tipo A/administração & dosagem
Toxinas Botulínicas Tipo A/efeitos adversos
Paralisia Cerebral/tratamento farmacológico
Seres Humanos
Injeções Subcutâneas
Letargia/induzido quimicamente
Masculino
Meclizina/uso terapêutico
Náusea/induzido quimicamente
Fármacos Neuromusculares/administração & dosagem
Fármacos Neuromusculares/efeitos adversos
Glândulas Salivares
Hidrobrometo de Escopolamina/administração & dosagem
Sialorreia/etiologia
Síndrome de Abstinência a Substâncias/complicações
Síndrome de Abstinência a Substâncias/tratamento farmacológico
Adesivo Transdérmico
Resultado do Tratamento
Vômito/induzido quimicamente
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiemetics); 0 (Neuromuscular Agents); 3L5TQ84570 (Meclizine); 451IFR0GXB (Scopolamine Hydrobromide); EC 3.4.24.69 (Botulinum Toxins, Type A)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170830
[Lr] Data última revisão:
170830
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170113
[St] Status:MEDLINE
[do] DOI:10.1097/PHM.0000000000000665


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[PMID]:27789115
[Au] Autor:Shih RD; Walsh B; Eskin B; Allegra J; Fiesseler FW; Salo D; Silverman M
[Ad] Endereço:Department of Integrated Medical Science, Charles E. Schmidt College of Medicine, Florida Atlantic University, Boca Raton, Florida.
[Ti] Título:Diazepam and Meclizine Are Equally Effective in the Treatment of Vertigo: An Emergency Department Randomized Double-Blind Placebo-Controlled Trial.
[So] Source:J Emerg Med;52(1):23-27, 2017 Jan.
[Is] ISSN:0736-4679
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Vertigo is a debilitating disease that is commonly encountered in the emergency department (ED). Diazepam and meclizine are oral medications that are commonly used to alleviate symptoms. OBJECTIVES: We sought to determine whether meclizine or diazepam is superior in the treatment of patients with peripheral vertigo in the ED. METHODS: We performed a double-blind clinical trial at a suburban, teaching ED. We randomized a convenience sample of adult patients with acute peripheral vertigo (APV) to diazepam 5 mg or meclizine 25 mg orally. Demographic and historical features were recorded on a standardized data form. Patients recorded their initial level (t0) of vertigo on a 100-mm visual analog scale (VAS) and after 30 min (t30) and 60 min (t60). The primary outcome parameter was the mean change in VAS score from t0 to t60. Differences between groups and 95% confidence intervals were calculated. Our a priori power calculation estimated that a sample size of 20 patients in each group was required to have an 80% power to detect a difference of 20 mm between treatment groups. RESULTS: There were 20 patients in the diazepam group and 20 in the meclizine group. The two groups were similar with respect to patient demographics and presenting signs and symptoms. At t60, the mean improvements in the diazepam and meclizine groups were 36 and 40, respectively (difference -4; 95% confidence interval -20 to 12; p = 0.60). CONCLUSION: We found no difference between oral diazepam and oral meclizine for the treatment of ED patients with acute peripheral vertigo.
[Mh] Termos MeSH primário: Diazepam/farmacologia
Meclizina/farmacologia
Resultado do Tratamento
Vertigem/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Diazepam/uso terapêutico
Método Duplo-Cego
Serviço Hospitalar de Emergência/organização & administração
Serviço Hospitalar de Emergência/estatística & dados numéricos
Feminino
Seres Humanos
Masculino
Meclizina/uso terapêutico
Meia-Idade
Estudos Prospectivos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
3L5TQ84570 (Meclizine); Q3JTX2Q7TU (Diazepam)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161030
[St] Status:MEDLINE


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[PMID]:27767902
[Au] Autor:Matsushita M; Mishima K; Esaki R; Ishiguro N; Ohno K; Kitoh H
[Ad] Endereço:Division of Neurogenetics, Center for Neurological Diseases and Cancer, and.
[Ti] Título:Maternal administration of meclozine for the treatment of foramen magnum stenosis in transgenic mice with achondroplasia.
[So] Source:J Neurosurg Pediatr;19(1):91-95, 2017 Jan.
[Is] ISSN:1933-0715
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE Achondroplasia (ACH) is the most common short-limbed skeletal dysplasia caused by gain-of-function mutations in the fibroblast growth factor receptor 3 (FGFR3) gene. Foramen magnum stenosis (FMS) is one of the serious neurological complications in ACH. Through comprehensive drug screening, the authors identified that meclozine, an over-the-counter drug for motion sickness, inhibited activation of FGFR3 signaling. Oral administration of meclozine to the growing ACH mice promoted longitudinal bone growth, but it did not prevent FMS. In the current study, the authors evaluated the effects of maternal administration of meclozine on FMS in ACH mice. METHODS The area of the foramen magnum was measured in 17-day-old Fgfr3 mice and wild-type mice using micro-CT scanning. Meclozine was administered to the pregnant mice carrying Fgfr3 offspring from embryonic Day (ED) 14.5 to postnatal Day (PD) 4.5. Spheno-occipital and anterior intraoccipital synchondroses were histologically examined, and the bony bridges were scored on PD 4.5. In wild-type mice, tissue concentrations of meclozine in ED 17.5 fetuses and PD 6.5 pups were investigated. RESULTS The area of the foramen magnum was significantly smaller in 17-day-old Fgfr3 mice than in wild-type mice (p < 0.005). There were no bony bridges in the spheno-occipital and anterior intraoccipital synchondroses in wild-type mice, while some of the synchondroses prematurely closed in untreated Fgfr3 mice at PD 4.5. The average bony bridge score in the cranial base was 7.053 ± 1.393 in untreated Fgfr3 mice and 6.125 ± 2.029 in meclozine-treated Fgfr3 mice. The scores were not statistically significant between mice with and those without meclozine treatment (p = 0.12). The average tissue concentration of meclozine was significantly higher (508.88 ± 205.16 ng/g) in PD 6.5 mice than in ED 17.5 mice (56.91 ± 20.05 ng/g) (p < 0.005). CONCLUSIONS Maternal administration of meclozine postponed premature closure of synchondroses in some Fgfr3 mice, but the effect on preventing bony bridge formation was not significant, probably due to low placental transmission of the drug. Meclozine is likely to exhibit a marginal effect on premature closure of synchondroses at the cranial base in ACH.
[Mh] Termos MeSH primário: Acondroplasia/diagnóstico por imagem
Acondroplasia/tratamento farmacológico
Forame Magno/diagnóstico por imagem
Troca Materno-Fetal/efeitos dos fármacos
Meclizina/administração & dosagem
[Mh] Termos MeSH secundário: Acondroplasia/genética
Animais
Constrição Patológica/diagnóstico por imagem
Constrição Patológica/tratamento farmacológico
Constrição Patológica/genética
Feminino
Forame Magno/efeitos dos fármacos
Exposição Materna
Troca Materno-Fetal/fisiologia
Camundongos
Camundongos Transgênicos
Gravidez
Distribuição Aleatória
Receptor Tipo 3 de Fator de Crescimento de Fibroblastos/antagonistas & inibidores
Receptor Tipo 3 de Fator de Crescimento de Fibroblastos/genética
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
3L5TQ84570 (Meclizine); EC 2.7.10.1 (FGFR3 protein, human); EC 2.7.10.1 (Receptor, Fibroblast Growth Factor, Type 3)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161022
[St] Status:MEDLINE
[do] DOI:10.3171/2016.7.PEDS16199


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[PMID]:27450607
[Au] Autor:Banting J; Meriano T
[Ti] Título:Sea State Green.
[So] Source:J Spec Oper Med;16(2):78-81, 2016.
[Is] ISSN:1553-9768
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The series objective is to review various clinical conditions/ presentations, including the latest evidence on management, and to dispel common myths. In the process, core knowledge and management principles are enhanced. A clinical case will be presented. Cases will be drawn from real life but phrased in a context that is applicable to the Special Operations Forces (SOF) or tactical emergency medical support (TEMS) environment. Details will be presented in such a way that the reader can follow along and identify how they would manage the case clinically depending on their experience and environment situation. Commentary will be provided by currently serving military medical technicians. The medics and author will draw on their SOF experience to communicate relevant clinical concepts pertinent to different operational environments including SOF and TEMS. Commentary and input from active special op.
[Mh] Termos MeSH primário: Acupressão/métodos
Antieméticos/uso terapêutico
Antagonistas Colinérgicos/uso terapêutico
Antagonistas de Dopamina/uso terapêutico
Antagonistas dos Receptores Histamínicos/uso terapêutico
Enjoo devido ao Movimento/prevenção & controle
[Mh] Termos MeSH secundário: Auxiliares de Emergência
Seres Humanos
Meclizina/uso terapêutico
Metoclopramida/uso terapêutico
Militares
Enjoo devido ao Movimento/fisiopatologia
Enjoo devido ao Movimento/terapia
Ondansetron/uso terapêutico
Prometazina/uso terapêutico
Hidrobrometo de Escopolamina/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antiemetics); 0 (Cholinergic Antagonists); 0 (Dopamine Antagonists); 0 (Histamine Antagonists); 3L5TQ84570 (Meclizine); 451IFR0GXB (Scopolamine Hydrobromide); 4AF302ESOS (Ondansetron); FF28EJQ494 (Promethazine); L4YEB44I46 (Metoclopramide)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170202
[Lr] Data última revisão:
170202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160725
[St] Status:MEDLINE


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[PMID]:26501107
[Au] Autor:Kishi S; Campanholle G; Gohil VM; Perocchi F; Brooks CR; Morizane R; Sabbisetti V; Ichimura T; Mootha VK; Bonventre JV
[Ad] Endereço:Renal Division, Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.
[Ti] Título:Meclizine Preconditioning Protects the Kidney Against Ischemia-Reperfusion Injury.
[So] Source:EBioMedicine;2(9):1090-101, 2015 Sep.
[Is] ISSN:2352-3964
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Global or local ischemia contributes to the pathogenesis of acute kidney injury (AKI). Currently there are no specific therapies to prevent AKI. Potentiation of glycolytic metabolism and attenuation of mitochondrial respiration may decrease cell injury and reduce reactive oxygen species generation from the mitochondria. Meclizine, an over-the-counter anti-nausea and -dizziness drug, was identified in a 'nutrient-sensitized' chemical screen. Pretreatment with 100 mg/kg of meclizine, 17 h prior to ischemia protected mice from IRI. Serum creatinine levels at 24 h after IRI were 0.13 ± 0.06 mg/dl (sham, n = 3), 1.59 ± 0.10 mg/dl (vehicle, n = 8) and 0.89 ± 0.11 mg/dl (meclizine, n = 8). Kidney injury was significantly decreased in meclizine treated mice compared with vehicle group (p < 0.001). Protection was also seen when meclizine was administered 24 h prior to ischemia. Meclizine reduced inflammation, mitochondrial oxygen consumption, oxidative stress, mitochondrial fragmentation, and tubular injury. Meclizine preconditioned kidney tubular epithelial cells, exposed to blockade of glycolytic and oxidative metabolism with 2-deoxyglucose and NaCN, had reduced LDH and cytochrome c release. Meclizine upregulated glycolysis in glucose-containing media and reduced cellular ATP levels in galactose-containing media. Meclizine inhibited the Kennedy pathway and caused rapid accumulation of phosphoethanolamine. Phosphoethanolamine recapitulated meclizine-induced protection both in vitro and in vivo.
[Mh] Termos MeSH primário: Precondicionamento Isquêmico
Rim/irrigação sanguínea
Rim/patologia
Meclizina/uso terapêutico
Substâncias Protetoras/uso terapêutico
Traumatismo por Reperfusão/tratamento farmacológico
[Mh] Termos MeSH secundário: Lesão Renal Aguda/complicações
Lesão Renal Aguda/tratamento farmacológico
Lesão Renal Aguda/patologia
Trifosfato de Adenosina/metabolismo
Animais
Respiração Celular/efeitos dos fármacos
Citocromos c/metabolismo
Desoxiglucose/farmacologia
Modelos Animais de Doenças
Células Epiteliais/efeitos dos fármacos
Células Epiteliais/patologia
Etanolaminas/metabolismo
Galactose/farmacologia
Glicólise/efeitos dos fármacos
Seres Humanos
Inflamação/complicações
Inflamação/patologia
Rim/efeitos dos fármacos
Túbulos Renais/efeitos dos fármacos
Túbulos Renais/metabolismo
Túbulos Renais/patologia
L-Lactato Desidrogenase/metabolismo
Células LLC-PK1
Masculino
Meclizina/farmacologia
Meclizina/toxicidade
Camundongos Endogâmicos C57BL
Mitocôndrias/efeitos dos fármacos
Mitocôndrias/metabolismo
Mitocôndrias/ultraestrutura
Substâncias Protetoras/farmacologia
Traumatismo por Reperfusão/complicações
Traumatismo por Reperfusão/patologia
Cianeto de Sódio/farmacologia
Suínos
Regulação para Cima/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Ethanolamines); 0 (Protective Agents); 3L5TQ84570 (Meclizine); 78A2BX7AEU (phosphorylethanolamine); 8L70Q75FXE (Adenosine Triphosphate); 9007-43-6 (Cytochromes c); 9G2MP84A8W (Deoxyglucose); EC 1.1.1.27 (L-Lactate Dehydrogenase); O5DDB9Z95G (Sodium Cyanide); X2RN3Q8DNE (Galactose)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:170615
[Lr] Data última revisão:
170615
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151027
[St] Status:MEDLINE
[do] DOI:10.1016/j.ebiom.2015.07.035


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[PMID]:26501091
[Au] Autor:Rongen GA
[Ad] Endereço:Department of Pharmacology and Toxicology, Radboud university medical center, P.O. Box 9101, 6500 HB Nijmegen, The Netherlands.
[Ti] Título:High Dose Meclizine Prevents Renal Ischemia-Reperfusion Injury in Healthy Male Mice.
[So] Source:EBioMedicine;2(9):1012-3, 2015 Sep.
[Is] ISSN:2352-3964
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Mh] Termos MeSH primário: Meclizina
Traumatismo por Reperfusão/prevenção & controle
[Mh] Termos MeSH secundário: Lesão Renal Aguda/prevenção & controle
Animais
Rim
Masculino
Camundongos
[Pt] Tipo de publicação:COMMENT; EDITORIAL
[Nm] Nome de substância:
3L5TQ84570 (Meclizine)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151027
[St] Status:MEDLINE
[do] DOI:10.1016/j.ebiom.2015.09.016


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[PMID]:26456247
[Au] Autor:Zhao Y; Quan P; Fang L
[Ad] Endereço:Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
[Ti] Título:Preparation of an oral thin film containing meclizine hydrochloride: In vitro and in vivo evaluation.
[So] Source:Int J Pharm;496(2):314-22, 2015 Dec 30.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Oral thin film (OTF) is a preparation of postage stamp size, with advantages of flexible, tasty and without water for oral administration. A commercial product (Zentrip®) was developed for people who suffered from motion sickness. In order to improve the mechanical strength of Zentrip®, OTF containing meclizine hydrochloride (MH) was designed and prepared using the solvent casting method. The characteristics of the prepared OTF were evaluated using micrometer, auto stripping tester, DSC, X-ray diffraction. ATR-FTIR was employed to investigate the interaction between drug and polymer. The thickness of MH OTF obtained was 0.116±0.004mm, the tensile strength was 17.37±1.54Nmm(-2) and the drug dissolution at 5min was more than 80% both in distilled water and 0.1mol/L HCL. DSC and XRD showed MH was amorphous in the polymer. ATR-FTIR indicated the MH molecules inserted into the network structure of polymer, which resulted in an inhibition of drug recrystallization. The Cmax of Zentrip® and MH OTF were 1.46±0.44µg/mL and 1.91±0.51µg/mL, and the AUC were 10.38±2.93µgh/mL and 13.74±3.23µgh/mL, respectively. Compared with Zentrip®, MH OTF successfully overcome the weakness of mechanical strength, possessed faster dissolution profile and showed bioequivalence in pharmacokinetics, deserving to a further development.
[Mh] Termos MeSH primário: Portadores de Fármacos/administração & dosagem
Portadores de Fármacos/síntese química
Meclizina/administração & dosagem
Meclizina/síntese química
[Mh] Termos MeSH secundário: Administração Oral
Animais
Portadores de Fármacos/metabolismo
Composição de Medicamentos/métodos
Avaliação Pré-Clínica de Medicamentos/métodos
Masculino
Meclizina/sangue
Ratos
Ratos Wistar
Resistência à Tração/fisiologia
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 3L5TQ84570 (Meclizine)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151221
[Lr] Data última revisão:
151221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151013
[St] Status:MEDLINE


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[PMID]:26239802
[Au] Autor:Foo WY; Tay HY; Chan EC; Lau AJ
[Ad] Endereço:Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore. Electronic address: winnie_foo@u.nus.edu.
[Ti] Título:Meclizine, a pregnane X receptor agonist, is a direct inhibitor and mechanism-based inactivator of human cytochrome P450 3A.
[So] Source:Biochem Pharmacol;97(3):320-30, 2015 Oct 01.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Meclizine is an agonist of human pregnane X receptor (PXR). It increases CYP3A4 mRNA expression, but decreases CYP3A-catalyzed testosterone 6ß-hydroxylation in primary cultures of human hepatocytes, as assessed at 24h after the last dose of meclizine. Therefore, the hypothesis to be tested is that meclizine inactivates human CYP3A enzymes. Our findings indicated that meclizine directly inhibited testosterone 6ß-hydroxylation catalyzed by human liver microsomes, recombinant CYP3A4, and recombinant CYP3A5. The inhibition of human liver microsomal testosterone 6ß-hydroxylation by meclizine occurred by a mixed mode and with an apparent Ki of 31±6µM. Preincubation of meclizine with human liver microsomes and NADPH resulted in a time- and concentration-dependent decrease in testosterone 6ß-hydroxylation. The extent of inactivation required the presence of NADPH, was unaffected by nucleophilic trapping agents or reactive oxygen species scavengers, attenuated by a CYP3A substrate, and not reversed by dialysis. Meclizine selectively inactivated CYP3A4, but not CYP3A5. In contrast to meclizine, which has a di-substituted piperazine ring, norchlorcyclizine, which is a N-debenzylated meclizine metabolite with a mono-substituted piperazine ring, did not inactivate but directly inhibited hepatic microsomal CYP3A activity. In conclusion, meclizine inhibited human CYP3A enzymes by both direct inhibition and mechanism-based inactivation. In contrast, norchlorcyclizine is a direct inhibitor but not a mechanism-based inactivator. Furthermore, a PXR agonist may also be an inhibitor of a PXR-regulated enzyme, thereby giving rise to opposing effects on the functional activity of the enzyme and indicating the importance of measuring the catalytic activity of nuclear receptor-regulated enzymes.
[Mh] Termos MeSH primário: Inibidores do Citocromo P-450 CYP3A/farmacologia
Citocromo P-450 CYP3A/metabolismo
Meclizina/farmacologia
Receptores de Esteroides/agonistas
[Mh] Termos MeSH secundário: Inibidores do Citocromo P-450 CYP3A/química
Relação Dose-Resposta a Droga
Seres Humanos
Técnicas In Vitro
Cinética
Meclizina/química
Microssomos Hepáticos/efeitos dos fármacos
Microssomos Hepáticos/enzimologia
Modelos Biológicos
Estrutura Molecular
Piperazinas/química
Piperazinas/farmacologia
Proteínas Recombinantes
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cytochrome P-450 CYP3A Inhibitors); 0 (Piperazines); 0 (Receptors, Steroid); 0 (Recombinant Proteins); 0 (pregnane X receptor); 3L5TQ84570 (Meclizine); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP3A); T875VN0D6E (norchlorcyclizine)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:150921
[Lr] Data última revisão:
150921
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150805
[St] Status:MEDLINE



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